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Design, Synthesis, Radiolabeling, and Biologic Evaluation of Three 18F-Fdg-Radiolabeled Targeting Peptides for the Imaging of Apoptosis Publisher Pubmed



Khoshbakht S1 ; Beiki D2 ; Geramifar P2 ; Kobarfard F3 ; Sabzevari O4 ; Amini M5 ; Bolourchian N6 ; Shamshirian D7 ; Shahhosseini S8
Authors
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Authors Affiliations
  1. 1. Shohada-E-Tajrish Hospital, School of Medicine, Shahid Behesti University of Medical Sciences, Tehran, Iran
  2. 2. Research Center for Nuclear Medicine, Tehran University of Medical Sciences, Tehran, Iran
  3. 3. Department of Pharmaceutical Chemistry and Radiopharmacy, School of Pharmacy, Phytochemistry Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran
  4. 4. Department of Toxicology and Pharmacology, Faculty of Pharmacy, Toxicology and Poisoning Research Centre, Tehran University of Medical Sciences, Tehran, Iran
  5. 5. Department of Medicinal Chemistry, Faculty of Pharmacy, Drug Design and Development Research Center, Tehran University of Medical Sciences, Tehran, Iran
  6. 6. Department of Pharmaceutics, Shahid Beheshti University of Medical Sciences, Tehran, Iran
  7. 7. PET/CT Center, Masih Daneshvari Hospital, Shahid Beheshti University of Medical Sciences, Tehran, Iran
  8. 8. Department of Pharmaceutical Chemistry and Radiopharmacy, School of Pharmacy, Protein Technology Research Center, Shahid Behesti University of Medical Sciences, Vali-e Asr Avenue, Niayesh Junction, Tehran, 14155-6153, Iran

Source: Cancer Biotherapy and Radiopharmaceuticals Published:2019


Abstract

Background: Early detection of apoptosis is very important for therapy and follow-up treatment in various pathologic conditions. Annexin V interacts strongly and specifically with phosphatidylserine, specific biomarkers of apoptosis with some limitations. Small peptides are suitable alternatives to annexin V. A reliable and noninvasive in vivo technique for the detection of apoptosis is in great demand. Based on our previous studies, three new peptide analogs of LIKKPF (Leu-Ile-Lys-Lys-Pro-Phe) as apoptosis imaging agents were developed. Materials and Methods: Aoa-LIKKP-Cl-F, Aoe-LIKKP-Pyr-F, and Aoe-LIKKP-Nap-F were synthesized, functionalized with aminooxy, and radiolabeled with 18F-FDG. Their biologic properties were evaluated in vitro using apoptotic Jurkat cells. 18F-FDG-Aoe-LIKKP-Pyr-F peptide was injected into normal and apoptotic mice models for biodistribution and in vivo positron emission tomography/computed tomography imaging studies. Results: 18F-FDG-Aoe-LIKKP-Pyr-F peptide showed higher affinity for apoptotic cells. The localization of peptide in apoptotic liver mice was confirmed in biodistribution and imaging studies. Conclusion: The results showed that Aoe-LIKKP-Pyr-F peptide is an auspicious agent for molecular imaging of apoptosis. © Copyright 2019, Mary Ann Liebert, Inc., publishers 2019.
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